“…Compounds 78 , 80 and 82 demonstrated high antiproliferative activities against SMMC-7721 cells with IC 50 values of 2.54, 2.69 and 2.31 μM ( Figure 43 ). All the tested compounds showed a weak cytotoxic effect against the normal cell line L929 [ 50 ].…”
Section: Derivatives Of 25-disubstituted-134-thiadiazolementioning
During recent years, small molecules containing five-member heterocyclic moieties have become the subject of considerable growing interest for designing new antitumor agents. One of them is 1,3,4-thiadiazole. This study is an attempt to collect the 1,3,4-thiadiazole and its derivatives, which can be considered as potential anticancer agents, reported in the literature in the last ten years.
“…Compounds 78 , 80 and 82 demonstrated high antiproliferative activities against SMMC-7721 cells with IC 50 values of 2.54, 2.69 and 2.31 μM ( Figure 43 ). All the tested compounds showed a weak cytotoxic effect against the normal cell line L929 [ 50 ].…”
Section: Derivatives Of 25-disubstituted-134-thiadiazolementioning
During recent years, small molecules containing five-member heterocyclic moieties have become the subject of considerable growing interest for designing new antitumor agents. One of them is 1,3,4-thiadiazole. This study is an attempt to collect the 1,3,4-thiadiazole and its derivatives, which can be considered as potential anticancer agents, reported in the literature in the last ten years.
“…The final compounds were purified, and their structures were characterized by spectroscopic methods ( 1 H-NMR, 13 C-NMR, and LC-MS/MS). In the 1 H NMR spectrum, monosubstituted benzene protons had triplet and doublet peaks between 6.98 ppm and 7.56 ppm.…”
Section: Chemistrymentioning
confidence: 99%
“…In addition to structure elucidations using routine spectroscopic methods, 2D NMR studies including 1 H- 13 C HMBC and 1 H-13 C HSQC were performed for compound 4a, as seen in Figure 1 information obtained in the HSQC, the peak at 31.49 ppm belongs to the methyl carbon and the peak at 38.86 ppm belongs to the methylene carbon. HMBC shows interactions between hydrogen and carbon at a distance of 2 to 4 bonds.…”
Section: Chemistrymentioning
confidence: 99%
“…The potential anticancer activity of this structure is one the most interesting areas that have encouraged researchers to focus on it. Hence, a large number of 1,3,4-thiadiazole derivatives have been synthesized and their molecular mechanism of anticancer activity has been investigated [10][11][12][13][14][15].…”
Cancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.
To obtain new anticancer agents with antimetastatic adjunct efficacy, a series of novel N 4 -hydrazone derivatives of 5,7-dihydro-6H-pyrrolo [2,3-d]pyrimidin-6-one were designed and synthesized by an eight-step reaction, with appropriate yields. All the synthesized compounds were evaluated for their antiproliferative activity against A549 and MCF-7 cells and for antiplatelet aggregation activity in vitro. The results showed that compounds 25 and 35 not only showed potent antiproliferative activity against the A549 (IC 50 = 15.3 and 21.4 μM) and MCF-7 (IC 50 = 15.6 and 10.9 μM) cell lines but also showed certain antiplatelet aggregation activity (inhibition rates: 47.0% and 45.8%).These results indicated that the structural modification on the N 4 -hydrazone moiety of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one is promising to obtain novel anticancer compounds with antimetastatic adjunct efficacy. In addition, a molecular docking study was performed to investigate the possible targets, and these results indicated that compounds 25 and 35 have the potential to target EGFR, HER2, and P2Y 12 .
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